In vitro and in vivo acetylcholinesterase-inhibiting effect of new classes of organophosphorus compounds


OZMEN M., SENER S., METE A., Kucukbay H.

ENVIRONMENTAL TOXICOLOGY AND CHEMISTRY, cilt.18, sa.2, ss.241-246, 1999 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 18 Sayı: 2
  • Basım Tarihi: 1999
  • Doi Numarası: 10.1002/etc.5620180221
  • Dergi Adı: ENVIRONMENTAL TOXICOLOGY AND CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.241-246
  • İnönü Üniversitesi Adresli: Evet

Özet

Anticholinesterase properties of 14 new synthesized organophosphorus (OP) compounds and four of their starting substances were tested in vitro and in vivo using electric eel acetylcholinesterase (AChE) and Rana ridibunda (frog of lowland) tadpoles, respectively. Gusathion-M(R) was used as a reference anti-AChE agent. Acetylcholinesterase inhibition capacity of tested compounds was assayed for 30-min period in vitro studies using electric eel AChE, of which 14 OP compounds inhibited enzyme activity more than 50% within 30 min, excluding Gusathion-M. However, four of the compounds inhibited AChE less than 50% during the test period. On the other hand, 12 of the OPs did not bring about mortality, whereas six of the tested compounds were found to be lethal agents for R. ridibunda tadpoles, for which values of concentration causing 50% lethality ranged from 14.42 to 89.95 ppm. Also, the highest degree of enzyme inhibition occurred by diethyl chlorophosphate (ETCP), which inhibited AChE activity 62% at 2.89 ppm in 24-h toxicity tests and which was more effective than Gusathion-M. The lethal OP compounds represented good correlation between dose and enzyme-inhibition capability in in vivo tests, but only ETCP showed such a relation for anti-AChE effect in both in vitro and in vivo conditions.